Abstract
Voltage-gated ion channels play a fundamental role in the generation and propagation of the cardiac action potential by acting synergistically to produce an ionic current across cellular membranes. Abnormalities of heart ion channel activities that lead to loss or gain of function (channelopathies) are often associated with disruption of the coordinated propagation of electrical activity of the cardiac myocytes and can generate fatal arrhythmogenesis. Drugs that act on cardiac ion channels have long been used to restore normal rhythm and conduction in patients affected by cardiac arrhythmias and offered to basic scientists the possibility to characterize distinct ion channel classes. This review will explore the mechanisms and role of the current anti-arrhythmic drugs used in the clinic, and discuss recent development on ion channel openers as potential anti-arrhythmic drugs.
Highlights
Voltage-gated ion channels (VGIC) are pore forming transmembrane proteins which are ion permeable and gated by changes of transmembrane voltage [1]
Opening and closing of VGIC expressed in cardiac myocytes generate and propagate the electric signal to shape the waveform of a cardiac action potential [2]
Closing of the Na+ channels in addition to the slow opening of Cl- [13,14,15] and potassium channels determines the initial descending deflection of the cardiac action potential [16]. This event is followed by a plateau in which an inward Ca2+ currents resulting from activation of L-type calcium channels [17,18,19] is balanced by an outward K+ current upon activation of Potassium Channel (KCNQ) and Potassium channel voltage gated subfamily H (KCNH) type potassium channels [16]
Summary
Current and Potential Antiarrhythmic Drugs Targeting Voltage-Gated Cardiac Ion Channels.
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